One Double Bond Between Ring Members Of The Five-membered Hetero Ring (i.e., Pyrrolines) Patents (Class 548/565)
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Patent number: 6399771Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, 2 and 3, to a plurality of processes for their preparation and to their use as pesticides.Type: GrantFiled: September 9, 2000Date of Patent: June 4, 2002Assignee: Bayer AktiengesellschaftInventors: Andrew Plant, Gerd Kleefeld, Thorsten Pötter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
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Patent number: 6391892Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)2CH3, CO(CH2)3CH3, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; and pharmaceutically acceptable salts thereof. The invention further provides pharmaceutical compositions containing compounds of formula I and methods of use for the compounds of formula I.Type: GrantFiled: March 10, 1995Date of Patent: May 21, 2002Assignee: Eli Lilly and CompanyInventors: Henry U. Bryant, Jeffrey A. Dodge
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Patent number: 6384053Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.Type: GrantFiled: March 10, 1995Date of Patent: May 7, 2002Assignee: Eli Lilly and CompanyInventor: Brian S. Muehl
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Patent number: 6372764Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: April 16, 2002Assignee: Merck & Co., Inc.Inventors: Jianming Bao, Robert K. Baker, William H. Parsons, Kathleen Rupprecht
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Patent number: 6369124Abstract: Aliphatic maleimides and methods using the same are disclosed. Polymerization of compositions which include the compounds of the invention may be activated by irradiating the composition with radiation.Type: GrantFiled: July 7, 1999Date of Patent: April 9, 2002Assignees: First Chemical Corporation, University of Southern MississippiInventors: Charles E. Hoyle, Shan Christopher Clark, E. Sonny Jönsson
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Patent number: 6362201Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.Type: GrantFiled: March 1, 2000Date of Patent: March 26, 2002Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, William H. Parsons, Kathleen Rupprecht
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Publication number: 20020026034Abstract: 1 The present invention ocncerns new amidinopyrroline derivatives of formula (I) with the meanings of the symbols as given in the description as well as a process for their production and their use in pharmaceutical preparations.Type: ApplicationFiled: June 8, 1998Publication date: February 28, 2002Inventors: RICHARD ENGH, SILVIA KONETSCHNY-RAPP, HANS-WILLI KRELL, MARTIN ULRICH, CHRISTOS TSAKLAKIDIS
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Patent number: 6307061Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.Type: GrantFiled: January 26, 2001Date of Patent: October 23, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Nitrosated and nitrosylated nonsteroidal antiinflammatory compounds, compositions and methods of use
Patent number: 6297260Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.Type: GrantFiled: October 29, 1999Date of Patent: October 2, 2001Assignee: NitroMed, Inc.Inventors: Upul K. Bandarage, Qing Dong, Xinqin Fang, David S. Garvey, Gregory J. Mercer, Stewart K. Richardson, Joseph D. Schroeder, Tiansheng Wang -
Patent number: 6294557Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.Type: GrantFiled: January 26, 2001Date of Patent: September 25, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6294569Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.Type: GrantFiled: January 26, 2001Date of Patent: September 25, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6274613Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, to a process for their preparation and to their use as pesticides.Type: GrantFiled: May 11, 1999Date of Patent: August 14, 2001Assignee: Bayer AktiengesellschaftInventors: Andrew Plant, Gerd Kleefeld, Thorsten Pötter, Christoph Erdelen, Norbert Mencke, Andreas Turberg, Ulrike Wachendorff-Neumann
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Patent number: 6265433Abstract: The present invention provides compounds having the structure: and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.Type: GrantFiled: May 14, 1999Date of Patent: July 24, 2001Assignee: G. D. Searle & CompanyInventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell, Julie Marion Miyashiro, James Malecha, Thomas Dale Penning
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Patent number: 6222064Abstract: A fluorination method of oxygen and halogen sites with diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating reagents is disclosed.Type: GrantFiled: January 14, 2000Date of Patent: April 24, 2001Assignee: Air Products and Chemicals, Inc.Inventors: Gauri Sankar Lal, Guido Peter Pez
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Patent number: 6207860Abstract: Diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating agents are disclosed.Type: GrantFiled: September 29, 1997Date of Patent: March 27, 2001Assignee: Air Products and Chemicals, Inc.Inventors: Gauri Sankar Lal, Guido Peter Pez, Reno Joseph Pesaresi, Jr.
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Patent number: 6201007Abstract: A compound of the following formula: and the salts thereof wherein A is hydrogen, halo, or hydroxy, broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.Type: GrantFiled: March 12, 1999Date of Patent: March 13, 2001Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo
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Patent number: 6166222Abstract: The invention relates to a process for preparing chiral 3,4-dehydroproline compounds of formula (I), in which R, R' and R" have the meanings given in the description. The invention is characterized by a pyrrolecarboxylic acid derivative compound of formula (II) reacted first with an alkali or alkaline earth metal in ammonia and then with an aqueous salt solution or a compound of formula (III) in which X is a leaving group to form the final chiral product compound.Type: GrantFiled: December 1, 1999Date of Patent: December 26, 2000Assignee: BASF AktiengesellschaftInventor: Bernd Schafer
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Patent number: 6156784Abstract: Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing ligands or receptors. Also disclosed are methods for preparing the compounds of the formula (I).Type: GrantFiled: December 7, 1999Date of Patent: December 5, 2000Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Rajashekhar Betageri, Jean-Marie Ferland, Montse Llinas-Brunet, Neil Moss, John R. Proudfoot
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Patent number: 6124472Abstract: 3-Pyrroline-2-carboxylic acid derivatives of the formula I ##STR1## are prepared by eliminating the sulfonic acid residue, with the aid of a base, from a compound of the formula II ##STR2##Type: GrantFiled: January 22, 1999Date of Patent: September 26, 2000Assignee: BASF AktiengesellschaftInventors: Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke, Friedhelm Balkenhohl, Udo Lange
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Patent number: 6080886Abstract: A fluorination method of oxygen and halogen sites with diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating reagents is disclosed.Type: GrantFiled: September 29, 1997Date of Patent: June 27, 2000Assignee: Air Products and Chemicals, Inc.Inventors: Gauri Sankar Lal, Guido Peter Pez
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Patent number: 6066763Abstract: A process for preparing .alpha.-hydroxy acids by heating ammonium salts of .alpha.-hydroxy acids of general formula (I), removing the formed ammonia and water, adding water to the residue, and heating the obtained mixture, wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, alkyl(C.sub.1 -C.sub.6)thioalkyl (C.sub.1 -C.sub.6), phenyl or the like. This process is freed from the problem of disposal of by-products such as ammonium bisulfate and makes it possible to prepare a free .alpha.-hydroxy acid from an ammonium salt thereof economically and in a high yield.Type: GrantFiled: August 25, 1998Date of Patent: May 23, 2000Assignee: Nippon Soda Co., Ltd.Inventor: Koichi Hayakawa
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Patent number: 6057342Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.Type: GrantFiled: July 7, 1997Date of Patent: May 2, 2000Assignee: Dupont Pharmaceutical Co.Inventors: John Matthew Fevig, Donald Joseph Phillip Pinto, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 6017914Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides benzothiophene compounds, intermediates, formulations, and methods.Type: GrantFiled: September 3, 1997Date of Patent: January 25, 2000Assignee: Eli Lilly and CompanyInventors: Henry Uhlman Bryant, Michael John Martin, Ken Matsumoto
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Patent number: 6002003Abstract: Activating groups for cyanine dyes used to label chain terminators in nucleotide sequencing, based on N-hydroxyphthalimide, are disclosed. From these activating groups, activated dyes of the present Invention are prepared which react with the derivitized nucleotide chain terminators to give a labeled chain terminator of the present Invention. The activating groups of the present Invention allow the dye-chain terminator reaction to occur at a much higher yield and with much greater selectivity for the mono-substituted product, compared with the prior art.Type: GrantFiled: April 14, 1998Date of Patent: December 14, 1999Assignee: Beckman Instruments, Inc.Inventors: Gene G.-Y. Shen, Thomas S. Dobashi
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Patent number: 5998399Abstract: Method of treating or reducing the risk of human disease or condition in which the synthesis or oversynthesis of nitric oxide forms a contributory part wherein a therapeutically effective amount of the compound of formula (I) as defined in the specification is administered to a person suffering from or susceptible to such disease or condition.Type: GrantFiled: November 16, 1998Date of Patent: December 7, 1999Assignee: Astra AktiebolagInventors: James E. Macdonald, Robert Gentile, Robert J. Murray
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Patent number: 5929097Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.Type: GrantFiled: October 6, 1997Date of Patent: July 27, 1999Assignee: American Cyanamid CompanyInventors: Jeremy Ian Levin, Mila T. Du, Aranapakam Mudumbai Venkatesan, Frances Christy Nelson, Arie Zask, Yansong Gu
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Patent number: 5925654Abstract: The present invention provides compounds having the structure: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.Type: GrantFiled: March 12, 1997Date of Patent: July 20, 1999Assignee: G.D. Searle & Co.Inventors: Barbara Baosheng Chen, Helen Chen, Mark Andrew Russell, Julie Marion Miyashiro, James Malecha, Thomas Dale Penning
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Patent number: 5856309Abstract: Compound of formula (I) are disclosed ##STR1## as well as optically active isomers or pharmacologically acceptable salts thereof. The compounds are useful active ingredients in pharmaceutical compositions, and methods of treating osteoporosis, inflammation or diseases which are due to thromboembolic events. Compounds of formula (II) are also disclosed ##STR2## which are useful as starting compounds for preparing compounds of formula (I).Type: GrantFiled: April 14, 1997Date of Patent: January 5, 1999Assignee: Boehringer Mannheim GmbHInventors: Silvia Konetschny-Rapp, Hans-Willi Krell, Ulrich Martin, Richard Engh, Christos Tsaklakidis
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Patent number: 5780486Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 27, 1997Date of Patent: July 14, 1998Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
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Patent number: 5747523Abstract: The invention relates to substituted ethyl .alpha.,.alpha.-diarylmethyl ether derivatives and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, and methods of treating cocaine addiction and overdose, and diseases and conditions characterized by abnormal dopaminergic neurotransmission, using the same.Type: GrantFiled: January 24, 1996Date of Patent: May 5, 1998Assignee: Guilford Pharmaceuticals Inc.Inventor: Paul F. Jackson
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Patent number: 5688945Abstract: The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R.sup.3, R.sup.4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z--R.sup.5 wherein Z is selected from CH.sub.n, NH.sub.m, O, S, SO.sub.2 and CO wherein n=1 or 2; m=0 or 1 and R.sup.5 is selected from alkyl, aryl and fluoroalkyl; or R.sup.3 and R.sup.4 together form a saturated or unsaturated ring system Y--V--Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C.sub.1 -C.sub.3 alkylene or alkenylene, --N.dbd., --N.dbd.N-- and ##STR2## wherein R.sub.Type: GrantFiled: December 20, 1996Date of Patent: November 18, 1997Assignees: Astra Aktiebolag, The University of Maryland at BaltimoreInventors: Susanna Karin Maria Bjork, Birgitta Kristina Gotthammar, Mats Torbjorn Linderberg, Johan Per Luthman, Kerstin Margareta Irma Persson, Robert Schwarcz
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Patent number: 5663308Abstract: Organosilicon polymers, including crosslinked polymers and crosslinkable prepolymers, of cyclic polysiloxane, organic dyes, and, optionally, polyenes. The dyes include those with delocalized Pi electron systems linking electron donor groups and electron acceptor groups, and with at least two carbon-carbon double bond-containing pendant groups attached to at least two different sites from among the indicated delocalized Pi electron systems, donor groups, and acceptor groups.Type: GrantFiled: February 7, 1994Date of Patent: September 2, 1997Assignee: Hercules IncorporatedInventors: Wayne Michael Gibbons, Robert Paul Grasso, Michael Kevin O'Brien, Paul Joseph Shannon, Shao-Tang Sun
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Patent number: 5576431Abstract: A perfluoro-cyclic imine represented by the formula: ##STR1## is produced by a method which comprises placing in a reaction vessel a perfluoro compound represented by the formula: ##STR2## wherein X stands for one member selected from among CF.sub.2, CF(CF.sub.3), and oxygen atom, M for one member selected from among monovalent alkali metal ions and alkaline earth metal ions, and n for 0, 1, or 2 and heating the perfluoro compound to a temperature in the approximate range of 100.degree. C. to 500.degree. C.Type: GrantFiled: December 7, 1995Date of Patent: November 19, 1996Assignee: Agency of Industrial Science & Technology, Ministry of International Trade & IndustryInventors: Masakazu Nishida, Takashi Abe, Haruhiko Fukaya
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Patent number: 5525735Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.Type: GrantFiled: December 12, 1994Date of Patent: June 11, 1996Assignee: AFFYMAX Technologies NVInventors: Mark A. Gallop, Martin A. Murphy
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Patent number: 5525734Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds on solid supports and synthetic compound libraries comprising pyrrolidine groups prepared by such methods.Type: GrantFiled: June 22, 1994Date of Patent: June 11, 1996Assignee: Affymax Technologies N.V.Inventors: Mark A. Gallop, Martin A. Murphy
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Patent number: 5512290Abstract: A powder-form composition of 2-acetyl-1-pyrroline incorporated with a support of maltodextrin and/or cyclodextrin. The composition is prepared by hydrolyzing a 2-(1-alkoxyethenyl)-1-pyrroline with an acid to obtain a reaction medium, adding an equimolar amount of a base to the reaction medium to obtain a neutralized reaction medium containing 2-acetyl-1-pyrroline, combining maltodextrin and/or cyclodextrin with the neutralized reaction medium to obtain a support solution and freeze-drying the support solution to obtain the composition.Type: GrantFiled: December 27, 1994Date of Patent: April 30, 1996Assignee: Nestec S.A.Inventors: Philippe Duby, Tuong Huynh-Ba
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Patent number: 5489562Abstract: A herbicidal composition having acivicin, its derivatives or salts or combinations thereof as its active component.A process for controlling unwanted plants comprising applying a herbicidally effective amount of acivicin, its derivatives or salts or combinations thereof to the unwanted plant.Type: GrantFiled: July 13, 1994Date of Patent: February 6, 1996Assignee: Rohm and Haas CompanyInventors: Ernest L. Burdge, Lori A. Spangler
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Patent number: 5470921Abstract: A synthetic polyamide of formula I and its salts ##STR1## in which each R.sub.1 independently is selected from hydrogen, carboxyl, amino or a group of formula .alpha.-A.sub.1 -R.sub.10 (.alpha.)where A, is a bridging group and R.sub.10 is a sterically hindered amine group;each R.sub.2 independently is hydrogen or a group of formula .alpha.A is a bridging group of the formula ##STR2## is 0 or 1; R.sub.3 is hydrogen, C.sub.1-12 alkyl or is a significance of R.sub.10 ;R.sub.5 is hydrogen or C.sub.1-12 alkylR.sub.4 is a significance of R.sub.10 or a group of formula .alpha.; andp is an integer from 5 to 200;with the proviso that the compound of formula I contains 1-400 sterically hindered amine groups.Type: GrantFiled: May 20, 1994Date of Patent: November 28, 1995Assignee: Sandoz Ltd.Inventors: Bansi L. Kaul, Angelos-Elie Vougioukas, Jurgen Goldmann
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Patent number: 5463079Abstract: A process for preparing five-membered nitrogen heterocycles of the general formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 are hydrogen,R.sup.1 is C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.10 -hydroxyalkyl, C.sub.1 -C.sub.10 -aminoalkyl, aryl, C.sub.7 -C.sub.10 -aralkyl and C.sub.7 -C.sub.10 -alkylaryl,R.sup.5 and R.sup.6 are C.sub.1 -C.sub.8 -alkyl,R.sup.2 and R.sup.3 together are oxygen with the proviso that R.sup.8 is hydrogen,R.sup.3 and R.sup.4 and/or R.sup.7 and R.sup.8 or R.sup.4 and R.sup.7 together are a bond,comprises reacting vinyloxiranes of the general formula II ##STR2## where R.sup.5 and R.sup.6 have the abovementioned meanings, with ammonia or primary amines of the general formula IIIR.sup.1 --NH.sub.2 (III),where R.sup.1 has the abovementioned meanings, in the presence of a compound of an element of Group VIIIb or Ib of the Periodic Table, with or without the addition of a Lewis acid, at from 20.degree. to 200.degree. C.Type: GrantFiled: June 27, 1994Date of Patent: October 31, 1995Assignee: BASF AktiengesellschaftInventors: Rolf Pinkos, Rolf Fischer
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5446171Abstract: 2-acetyl-1-pyrroline is prepared by hydrolyzing a 2-(1-alkoxyethenyl)-1-pyrroline compound with an acid to obtain a reaction medium and then adding an equimolar amount of a base to the reaction medium to obtain a neutralized reaction medium containing 2-acetyl-1-pyrroline.Type: GrantFiled: December 27, 1994Date of Patent: August 29, 1995Assignee: Nestec S.A.Inventors: Philippe Duby, Tuong Huynh-Ba
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Patent number: 5424334Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions--of such phenyl amidines derivatives.Type: GrantFiled: December 19, 1991Date of Patent: June 13, 1995Assignee: G. D. Searle & Co.Inventors: Norman A. Abood, Robert B. Garland, Masateru Miyano
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Patent number: 5380876Abstract: There are provided important pyrroline and glycine intermediates, methods for the preparation of said intermediates and the use thereof in the manufacture of arylpyrrole insecticidal agents.Type: GrantFiled: November 22, 1993Date of Patent: January 10, 1995Assignee: American Cyanamid CompanyInventors: Robert F. Doehner, Jr., Jerry M. Barton, David G. Kuhn
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Patent number: 5330981Abstract: This application describes 3-arylalkyl esters of 4,5-dihydro-9,10-dioxo-2-anthracenecarboxylic acid and a process for making them. Also described is a method of using the compounds in the treatment of arthritis.Type: GrantFiled: December 30, 1992Date of Patent: July 19, 1994Assignee: Istituto Gentili S.p.A.Inventors: Sergio Rosini, Maurizio Mian
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Patent number: 5280127Abstract: 2-(1-alkoxyethenyl)-1-pyrroline compounds. The compounds may be employed for preparing food flavorant compositions, and 2-(1-ethoxyethenyl)-1-pyrroline, in particular, has characteristics suiting it as a flavoring agent for food products.Type: GrantFiled: November 20, 1992Date of Patent: January 18, 1994Assignee: Nestec S.A.Inventors: Philippe Duby, Tuong Huynh-Ba
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Patent number: 5276147Abstract: The subject of the present invention is compounds which correspond to the following general formula: ##STR1## in which R.sub.1 and R.sub.3 independently of one another represent H, an alkyl, alkenyl, cycloalkyl, aryl, arylalkyl or an alkylaryl group, a heterocycle, or groups which are unsubstituted or substituted, in particular by one or more hydroxyl or alkoxy groups or halogen;n represents an integer from 1 to 5;i in each case takes values from 1 to n for the n successive ##STR2## links; R.sub.2, R.sub.4.sup.i and R.sub.5.sup.i independently of one another represent H, an alkyl, alkenyl, aryl, alkoxy, hydroxyalkyl, alkoxyalkyl, amido, acyl or carboxyalkyl group, or a salt, or an alkyl ester of the latter; or R.sub.4.sup.i and R.sub.5.sup.i together form an oxo group ##STR3## R.sub.6 and R.sub.7 represent H, or R.sub.6 and R.sub.7 together form an oxo group ##STR4## x represents a 5- or 6-membered heterocycle which contains at least one nitrogen atom, or, in the event that ##STR5## where R.sub.8 and R.sub.Type: GrantFiled: April 19, 1990Date of Patent: January 4, 1994Assignee: Medgenix Group S.A.Inventors: John R. Thornback, Marcel Deblaton, Gillian F. Morgan
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Patent number: 5187279Abstract: (-)-Swainsonine is prepared by the steps of first reacting a compound having the formula: ##STR1## wherein each R.sub.2 is lower alkyl, with (4-carbalkoxybutyl) triphenylphosphonium bromide in a strong base to obtain an alcohol having the formula: ##STR2## wherein R.sub.2 is as defined above and R is C.sub.1 -C.sub.8 alkyl; the alcohol is then reacted with methanesulfonyl chloride or p-toluenesulfonyl chloride or benzenesulfonyl chloride in the presence of a tertiary amine to obtain the corresponding sulfonate. Heating the sulfonate with an azide in an organic solvent yields an imine having the formula: ##STR3## wherein R.sub.2 and R are ad defined above. Treating the imine with an inorganic base, in aqueous alcohol provides upon acidification, the corresponding acid. Heating the acid at reflux temperature in organic solvent, yields an enamide having the formula: ##STR4## wherein R.sub.2 is as defined above.Type: GrantFiled: August 14, 1991Date of Patent: February 16, 1993Inventors: Jin K. Cha, Richard B. Bennett, III
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Patent number: 5120876Abstract: This invention relates to optical elements capable of second harmonic generation and novel compositions for use in such optical elements comprising polar molecules placed in noncentrosymmetric configuration wherein such optical element has an electron donor moiety linked through a conjugated bonding moiety to an electron acceptor moiety which consists of a selected fluorinated sulfone, fluorinated ketone, fluorinated vinyl sulfone or fluorinated alkyl vinyl sulfone.Type: GrantFiled: February 28, 1990Date of Patent: June 9, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventors: Lap T. Cheng, Andrew E. Feiring, Wilson Tam
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Patent number: 5118816Abstract: There are provided important pyrroline and glycine intermediates, methods for the preparation of these intermediates and their use in the manufacture of insecticidal, acaricidal and nematocidal arylpyrrole compounds. Illustrative of the pyrroline and glycine intermediates are compounds having the following structures: ##STR1## wherein A is hydrogen or C.sub.1 -C.sub.4 alkyl and W is CN, NO.sub.2 or CO.sub.2 R.sub.6.Type: GrantFiled: December 26, 1990Date of Patent: June 2, 1992Assignee: American Cyanamid CompanyInventors: Robert F. Doehner, Jr., Jerry M. Barton, David G. Kuhn
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Patent number: 5103007Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.Type: GrantFiled: October 27, 1989Date of Patent: April 7, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hiroaki Nomura, Hiroshi Akimoto, Keizo Inoue